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姜黄素载自乳化给药系统(cu-SEDDS):控制皮肤利什曼病原虫和继发细菌感染的有前景方法。

Curcumin-loaded self-emulsifying drug delivery system (cu-SEDDS): a promising approach for the control of primary pathogen and secondary bacterial infections in cutaneous leishmaniasis.

机构信息

Department of Biotechnology, Quaid-i-Azam University, Islamabad, Pakistan.

Institute of Basic Medical Sciences (IBMS), Khyber Medical University, Peshawar, Pakistan.

出版信息

Appl Microbiol Biotechnol. 2019 Sep;103(18):7481-7490. doi: 10.1007/s00253-019-09990-x. Epub 2019 Jul 12.

DOI:10.1007/s00253-019-09990-x
PMID:31300853
Abstract

Cutaneous leishmaniasis being a neglected tropical disease (NTD) faces several challenges in chemotherapy. If infected with secondary bacterial infections, the treatment regime of cutaneous ulcers in cutaneous leishmaniasis is further complicated which usually require two or more than two chemotherapeutic agents for healing. In the current study, seven curcumin-loaded self-emulsifying drug delivery system (cu-SEDDS) formulations (namely F1-F7) were prepared by mixing different excipients (oils, surfactants, and co-solvents) through stirring (vortex) and sonication. The formulations were characterized regarding their droplet size, polydispersity index (PDI), and zeta potential by zeta sizer. The cu-SEDDS formulations displayed different sizes ranging from 32.4 up to 80.0 nm. The zeta potential of the formulations ranged from - 1.56 up to - 4.8. The antileishmanial activities of the cu-SEDDS formulations in terms of IC against Leishmania tropica ranged from 0.19 up to 0.37 μg/ml. The minimum inhibitory concentrations (MICs) of these formulations against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Klebsiella pneumoniae were in the range of 48-62 μg/ml. The hemolysis caused by formulations was 1-2%. The spreading potential of the formulations (F1 and F5) over damaged skin model was remarkable. These results suggest that cu-SEDDS further enhanced the broad spectrum antileishmanial and antibacterial profile of curcumin and could be used for the treatment of cutaneous leishmaniasis and its associated secondary infections.

摘要

皮肤利什曼病是一种被忽视的热带病(NTD),在化疗方面面临着诸多挑战。如果感染了继发性细菌感染,皮肤利什曼病的皮肤溃疡的治疗方案就会更加复杂,通常需要两种或两种以上的化疗药物才能治愈。在目前的研究中,通过搅拌(涡旋)和超声处理,将不同的辅料(油、表面活性剂和共溶剂)混合制备了七种载姜黄素自乳化药物传递系统(cu-SEDDS)制剂(即 F1-F7)。通过zeta 粒径仪对制剂的粒径、多分散指数(PDI)和zeta 电位进行了表征。cu-SEDDS 制剂的粒径范围为 32.4 至 80.0nm。制剂的 zeta 电位范围为-1.56 至-4.8。cu-SEDDS 制剂对利什曼原虫的抗利什曼活性(以 IC 表示)范围为 0.19 至 0.37μg/ml。这些制剂对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和肺炎克雷伯菌的最小抑菌浓度(MIC)范围为 48-62μg/ml。制剂引起的溶血率为 1-2%。制剂(F1 和 F5)在受损皮肤模型上的扩散潜力显著。这些结果表明,cu-SEDDS 进一步增强了姜黄素的广谱抗利什曼和抗菌特性,可用于治疗皮肤利什曼病及其相关的继发性感染。

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